The present study aimed to investigate the effect of AZT derivates containing tellurium (Te) on human breast cancer cell lines and the mechanisms underlying cell death. The inhibitory effect of AZT and its derivatives (7m and 7r) was determined by the MTT assay (6.25, 12.5, 25, 50 and 100 μM in 24 and 48 h time points), meanwhile the induction of apoptosis and the cell cycle phases was investigated by flow cytometry. The MTT assay showed that AZT derivatives decreased the rate of cell proliferation at concentrations of 12.5 μM, while commercial AZT showed low antitumor potential. In flow cytometric analysis, we demonstrate that the AZT derivatives do not induce apoptosis at the concentration tested and promote the cell cycle arrest in the S phase. Besides, predicted absorption, distribution, metabolization, excretion and toxicity analysis suggest that the compounds possess a good pharmacokinetic profile and possibly less toxicity when compared to conventional AZT. These compounds containing tellurium in their formulation are potential therapeutic agents for breast cancer.

本研究旨在研究含碲（Te）的AZT衍生物对人乳腺癌细胞系的影响以及细胞死亡的潜在机制。AZT及其衍生物（7m和7r的抑制作用）。通过MTT测定（在24和48小时时间点分别为6.25、12.5、25、50和100μM）测定），同时通过流式细胞术研究细胞凋亡的诱导和细胞周期阶段。MTT分析表明，在浓度为12.5μM的条件下，AZT衍生物可降低细胞增殖速率，而商用AZT则显示出较低的抗肿瘤潜力。在流式细胞仪分析中，我们证明了AZT衍生物在所测试的浓度下不会诱导细胞凋亡，并促进了S期的细胞周期停滞。此外，预测的吸收，分布，代谢，排泄和毒性分析表明，与常规AZT相比，该化合物具有良好的药代动力学特征，且毒性可能更低。这些在制剂中含有碲的化合物是潜在的乳腺癌治疗剂。